Glucokinase (GK), also referred to as Hexokinase IV, is one of four hexokinases that are found in mammals. Hexokinases catalyze the first step in the metabolism of glucose, i.e., the conversion of glucose to glucose-6-phosphate. GK has been found to have a critical role in whole-body glucose homeostasis. As such, activation of GK represents a potentially important therapeutic intervention point and small molecule GK activators have considerable potential for the treatment or prophylaxis of metabolic diseases and disorders, for example, Type II diabetes.